Topical Composition for Pain Relief

ABSTRACT

A topical composition for nociceptive and neuropathic pain relief comprises several of menthol, camphor, methyl sulfonyl methane, lidocaine, arnica montana, Harpagophytum tincture, Emu oil, maqui powder, turmeric oil and in some embodiments methyl salicylate or capsaicin with Cannabis sativa.

BACKGROUND OF THE INVENTION

Many people suffer from pains including musculoskeletal conditions suchas soft tissue trauma and arthritis. Some bear the pain associated withthose conditions for prolonged periods. Treatment of musculoskeletalpain using traditional analgesics and anti-inflammatory drugs and knowncombinations of traditional analgesics anti-inflammatory drugs is notalways effective.

FIELD OF INVENTION

This invention relates to the medicinal/chemical arts and to thetreatment of nociceptive and neuropathic pain in humans.

DISCUSSION OF THE RELATED ART

Medications for the relief of pain may include analgesics andanti-inflammatories. However, compositions that include theseingredients along with local anesthetics and/or counterirritants are notwell known.

SUMMARY OF THE INVENTION

The present invention provides a topical cream useful for treatingnociceptive and neuropathic pain in humans.

In an embodiment, a composition includes by weight percent about 15% ofcounterirritant/analgesic methyl salycilate, 8% of anesthetic/analgesic,5% of skin permeator/anti-inflammatory, 3.0% ofanalgesic/anti-itch/counterirritant, 2.9% of analgesic, 2.5% ofanalgesic/anti-inflammatory, 2.0% of anesthetic, 1.5% of antioxidant. Invarious embodiments, the ingredients of this composition are varied in arange of plus or minus 50%; for example, the anesthetic/analgesic isvaried from 4% to 12%. In various embodiments, the ingredients of thiscomposition are varied in a range of plus or minus 40%, in a range ofplus or minus 30%, in a range of plus or minus 20%, in a range of plusor minus 10%, in a range of plus or minus 5%.

In an embodiment, a composition includes by weight percent about 8% ofanesthetic/analgesic menthol, 5% of anti-inflammatory/skin permeator,3.19% of analgesic, 3% of analgesic/anti-itch/counterirritant, 2.625% ofanalgesic/anti-inflammatory, 2% of anesthetic, 1.5% of antioxidant. Invarious embodiments, the ingredients of this composition are varied in arange of plus or minus 50%; for example, the anesthetic/analgesicingredient is varied from 4% to 12%. In various embodiments, theingredients of this composition are varied in a range of plus or minus40%, in a range of plus or minus 30%, in a range of plus or minus 20%,in a range of plus or minus 10%, in a range of plus or minus 5%.

BRIEF DESCRIPTION OF THE DRAWINGS

The present invention is described with reference to the accompanyingfigures. These figures, incorporated herein and forming part of thespecification, illustrate the present invention and, together with thedescription, further serve to explain the principles of the inventionand to enable a person skilled in the relevant art to make and use theinvention.

FIG. 1 shows an embodiment of the invention wherein methyl salicylate isa main ingredient.

FIG. 2 shows an embodiment of the invention where capsaicin and hemp oilare ingredients used in place of methyl salicylate.

FIG. 3 shows the purpose of the ingredients used in the invention.

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

The disclosure provided in the following pages describes examples ofsome embodiments of the invention. The designs, figures, anddescriptions are non-limiting examples of certain embodiments of theinvention. For example, other embodiments of the disclosed device may ormay not include the features described herein. Moreover, disclosedadvantages and benefits may apply to only certain embodiments of theinvention and should not be used to limit the disclosed inventions.

In an embodiment, the invention comprises the ingredients shown in Table1 below.

TABLE 1 Topical Composition For Pain Relief Ingredients In A FirstEmbodiment Supplier (Lot number) + ASA-150 gm Item Ingredients otherinformation % W/W batch (gm) 1 Methyl Salicylate Spectrum 15.00 22.5 2MSM (Methyl sulfonyl Source Naturals (SN1535 5.00 7.5 methane) REVK151)used by May 2020 3 Lidocaine Spectrum USP (IEC0028) Retest 2.00 3.0 dateJun. 17, 2019 4 Arnica Montana (Flower TerraVita (512592) Best 2.91 4.4extract) obtained from 5% Before April 2022 w/w of raw material(extracted amount along with propylene glycol for 150 gm of batch (gm))5 Ginger extract obtained Starwest Botanical (68499) 0.50 0.8 from 1%w/w of raw Ginger (extracted amount along with propylene glycol for 150gm of batch (gm)) 6 Harpagophytum tincture Bulk Supplements.com 2.50 3.8(Devils claw extract) 7 Menthol Spectrum (1EE0771) Exp. 8.00 12.0 Date:Apr. 13, 2018 8 Camphor Spectrum (2EC0027) Exp. 3.00 4.5 Date: Sep. 30,2019 9 Maqui powder extract South Life (MFDP2016-08) 1.53 2.3 (extractedamount along Packing date Feb. 29, 2016 with propylene glycol for 150 gmof batch (gm)) 10 Emu Oil PipingRock.com (6250) Exp. 0.20 0.3 Date: notavailable 11 Aloe Vera Bulk Supplements.com 1.00 1.5 (12E0916) Bestbefore Sep. 15, 2020 12 Piper nigrum (Black pepper) Eden gardern 0.080.1 oil 13 Curcuma Longa (Tumeric) Eden gardern 0.13 0.2 oil 14 Bergamotoil Dr Adorable Inc, Exp. Date 0.30 0.5 December 2018 15 Natural Saffronyellow color Color Maker (Mfg. date 0.20 0.3 Formula 3635C Jun. 21,2017) 16 Cream Base 56.66 86.49 TOTALS 100 150

The cream base referred to in Table 1 is shown in Table 2 below.

TABLE 2 Cream Base ASA- 150 gm Supplier (Lot number) + % batch ItemIngredients other information W/W (gm) 1 Stearic acid Spectrum NF(2FF0167) 16.00 24.0 2 Cetyl Alcohol USB (36653-82-4) 1.00 1.5 3Isopropyl Palmitate Spectrum NF (2F10111) 1.00 1.5 4 Propyl Paraben VWRUSP (1GA0299) 0.15 0.2 5 Sorbitan Spectrum NF (2FG0337) 5.00 7.5Monostearate 6 Methyl Paraben VWR (3197C372) 0.10 0.2 7 SorbitolSolution Spectrum USP (1GC1050) 3.00 4.5 (70%) 8 Polysorbate 60 SpectrumNF (L-15031-AP) 5.00 7.5 9 Cabopol 940 Lutriol 0.25 0.4 10 Purifiedwater q.s. In House 26.16 39.2 TOTALS 56.66 86.49

Manufacturing Procedure

In a first step, weigh specified amounts of MSM, emu oil, maqui powderextract, ginger extract, arnica montana flower extract, devils clawextract, Aloe vera, methyl paraben, sorbitol solution, polysorbate 60,carbopol 940 and purified water in a suitable glass container and heatto 80±5° C. on a heated water bath and stir the mixture to disperse themixture completely.

In a second step, weight and mix specified amounts of methyl salicylate,lidocaine, stearic acid, cetyl alcohol, isopropyl palmitate, propylparaben, Piper nigrum (black pepper) oil, Curcuma longa (tumeric) oil,and sorbitan monostearate separately in a suitable glass container andheat to 80±5° C. on a heated water bath. Stir the dispersion to mix allcomponents.

In a third step, mix the components of step-II with the components ofstep-I at 80±5° C. under continuous homogenization for 10-15 minutes.

In a fourth step, remove the mixture from the heated water bath, addspecified amount of menthol, camphor, natural saffron yellow colorformula 3635C and flavoring agent (bergamot mint oil) and stircontinuously to disperse them uniformly.

In a fifth step, add the cream base.

In a sixth step, when the temperature of the composition is just abovethe solidification, the formulation is poured in to the suitable welllabeled aluminum tubes. The final product is cooled down to roomtemperature, capped and stored at room temperature.

In an embodiment, the invention comprises the ingredients shown in Table3 below.

TABLE 3 Topical Composition For Pain Relief Ingredients In A SecondEmbodiment For 150 gm Supplier (Lot number) + batch non- ItemIngredients other information % W/W ASA (gm) 1 Capsaicin extractobtained from Starwest Botanical (70519) 0.28 0.4 0.75% raw materialExp. Date: Jun. 20, 2019 2 MSM (Methyl sulfonyl methane) Source Naturals(SN1535 5 7.5 REVK151) used by May 2020 3 Lidocaine Spectrum USP(IEC0028) Retest 2 3.0 date Jun. 17, 2019 4 Arnica Montana (Flowerextract) TerraVita (512592) Best 2.91 4.4 obtained from 5% w/w of rawBefore April 2022 material (extracted amount along with propylene glycolfor 150 gm of batch (gm)) 5 Ginger extract obtained from StarwestBotanical (68499) 0.5 0.8 1% w/w of raw Ginger (extracted Exp. Date: Notavailable amount along with propylene glycol for 150 gm of batch (gm)) 6Harpagophytum tincture (Devils Bulk Supplements.com 2.5 3.8 clawextract) obtained from 2.5% w/w of raw material* 7 Menthol Spectrum(1EE0771) Exp. 8 12.0 Date: Apr. 13, 2018 8 Camphor Spectrum (2EC0027)Exp. 3 4.5 Date: Sep. 30, 2019 9 Maqui powder extract South Life(MFDP2016-08) 1.53 2.3 (extracted amount along with Packing date Feb.29, 2016 propylene glycol for 150 gm of batch (gm)) 10 Emu OilPipingRock.com (6250) Exp. 0.2 0.3 Date: not available 11 Aloe Vera BulkSupplements.com 1 1.5 (12E0916) Best before Sep. 15, 2020 12 Pipernigrum (Black pepper) oil Eden gardern 0.075 0.1 13 Curcuma Longa(Tumeric) oil Eden gardern 0.125 0.2 14 Cannabis Sativa (Hemp) oil Edengardern 0.125 0.2 15 Bergamot oil Dr Adorable Inc, Exp. Date 0.3 0.5December 2018 16 Natural Saffron yellow color Color Maker (Mfg. date 0.20.3 Formula 3635C Jun. 21, 2017) 17 Cream Base 75.535 113.28 TOTALS 100150

The cream base referred to in Table 3 is shown in Table 2 above.

In some embodiments, the methyl salicylate listed in Table 1 is includedin the list of ingredients shown in Table 3 with or without thecapsaicin extract. The weight percent of this additional ingredient maybe 15% with the cream base reduced by a corresponding amount. If thecapsaicin extract is excluded, the cream base may be increased by acorresponding amount.

Manufacturing Procedure

In a first step, weigh specified amounts of MSM, emu oil, maqui powderextract, ginger extract, Arnica Montana Flower extract, devils clawextract, aloe vera, methyl paraben, sorbitol solution, polysorbate 60,carbopol 940 and purified water in a suitable glass container and heatto 80±5° C. on a heated water bath and stir the mixture to disperse themixture completely.

In a second step, weight and mix specified amounts of capsaicin extract,lidocaine, stearic acid, cetyl alcohol, isopropyl palmitate, propylparaben, Piper nigrum (black pepper) oil, Curcuma longa (tumeric) oil,Cannabis sativa (hemp) oil and sorbitan monostearate separately in asuitable glass container and heat to 80±5° C. on a heated water bath.Stir the dispersion to mix all components.

In a third step, mix the components of step-II with the components ofstep-I at 80±5° C. under continuous homogenization for 10-15 minutes.

In a fourth step, remove the mixture from the heated water bath, addspecified amount of menthol, camphor, natural saffron yellow colorformula 3635C and flavoring agent (bergamot mint oil) and homogenizecontinuously to disperse them uniformly.

In a fifth step, add the cream base.

In a sixth step, when the temperature of the composition is just abovethe solidification, the formulation is poured in to the suitable welllabeled aluminum tubes. The final product is cooled down to roomtemperature, capped and stored at room temperature.

FIG. 1 shows the main ingredients 100 of a topical composition for painrelief used in an embodiment containing methyl salicylate. FIG. 2 showsthe main ingredients 200 of a topical composition for pain relief usedin an embodiment where hemp oil and capsaicin extract are used in placeof methyl salicylate. FIG. 3 shows the purpose 300 of each of thetopical composition for pain relief ingredients.

Experimental Results

It has been found that the composition can be used to treat generalizedmuscle and joint pain and inflammation. For example, the composition canbe used: as a topical anti-inflammatory to treat localize inflammation;as a moisturizer and conditioner for the skin as a secondary effect whenused for the purpose of reducing pain or inflammation as describedabove; in conjunction with other systemic anti-inflammatories as in agouty attack, resulting in significant reduction in pain andinflammation. Localized pain relief is provided for up to 4 to 6 hours.

Recommendations for Use

Pregnancy: Use not recommended in pregnancy. Consult with your Physicianprior to use.

Interactions: Consult with your Physician if on blood thinners, havekidney, liver or heart disease, and/or suffer from high blood pressure.Use only under the explicit guidance and approval of a physician if anyof the above conditions exist. Allergy: Do not use this product ifallergic to aspirin or to any of the active or inactive ingredientslisted on the package.

Caution: Do not use with alcohol or any other topical medication.Consult a physician or a pharmacist for possible cross-reactions orinteractions when taking or using other medications. Long-term use isnot recommended. Chronic use beyond 7 days should be done under thesupervision/guidance of a physician.

Application

For use, the composition is typically rubbed onto the skin in the areasof pain and/or inflammation, two or three times daily. Apply the creamto a small section of the affected area prior to more generalized use.Immediately stop using the cream and notify your Physician in the eventof any allergic or hypersensitivity reaction. If an allergic reactionsuch as a rash, hives or a more severe reaction occurs, consult amedical professional immediately or call 911 should the reaction appearto be life threatening.

What follows is a random selection of exemplary results. Pain levels arerecorded based on a scale of 1-3 low pain, 4-6 moderate pain, and 7-10severe pain. Inflammation levels are recorded based on a scale of 1 forno reduction in swelling to 10 for a profound reduction in swelling.Patients 1 and 2 were treated with the first embodiment of the topicalcomposition for pain relief. Other patients were treated with the secondembodiment of the topical composition for pain relief.

Patient 1: An adult male complained of chronic back pain. A severe painbaseline of 7 was determined before use of the topical composition forpain relief. Inflammatory response was not measured. After use of thecream, a moderate pain level of 4 was determined. No adverse sideeffects were observed.

Patient 2: An adult male complained of a right ankle bone bruise. Amoderate pain baseline of 5 was determined before use of the topicalcomposition for pain relief. After use of the cream, a low pain level of1 was determined along with an inflammation response of 3. No adverseside effects were observed.

Patient 3: An adult male complained of a wrist sprain. A moderate painbaseline of 6 was determined before use of the topical composition forpain relief. After use of the cream, a low pain level of 1 wasdetermined along with an inflammation response of 3. No adverse sideeffects were observed.

Patient 4: An adult male complained of Achilles tendonitis. A moderatepain baseline of 5 was determined before use of the topical compositionfor pain relief. After 3 days of use, applying the cream twice a day, alow pain level of 1 was determined along with an inflammation responseof 9. No side effects were observed.

Patient 5: An adult male complained of arthritis following knee surgeryand removal of a majority of the medial meniscus. A moderate painbaseline of 4 was determined before the use of the topical compositionfor pain relief. After three applications of the cream over a two dayperiod, the discomfort essentially disappeared and a pain level of 1 wasdetermined along with an inflammation response of 5. Side effect wasnoticeable smell of cream during first hour after application.

While various embodiments of the present invention have been describedabove, it should be understood that they have been presented by way ofexample only, and not limitation. It will be apparent to those skilledin the art that various changes in the form and details can be madewithout departing from the spirit and scope of the invention. As such,the breadth and scope of the present invention should not be limited bythe above-described exemplary embodiments, but should be defined only inaccordance with the following claims and equivalents thereof.

What is claimed is:
 1. A topical composition comprising, by weight: 10to 20% methyl salycilate; 6 to 12% anesthetic/analgesic; 4 to 8% skinpermeator/anti-inflammatory; 2 to 4%analgesic/anti-itch/counterirritant; 2 to 4% analgesic; 2 to 4%analgesic/anti-inflammatory; 1.4 to 2.6% anesthetic; and, 1 to 2%antioxidant.
 2. The composition of claim 1 where theanesthetic/analgesic is menthol.
 3. The composition of claim 2 where theskin permeator/anti-inflammatory is methyl sulfonyl methane.
 4. Thecomposition of claim 3 where the analgesic is Arnica montana.
 5. Thecomposition of claim 4 where the analgesic/anti-itch/counterirritant iscamphor.
 6. The composition of claim 5 where theanalgesic/anti-inflammatory is Harpagophytim tincture.
 7. Thecomposition of claim 6 where the anesthetic is lidocaine.
 8. Thecomposition of claim 7 where the antioxidant is maqui powder.
 9. Atopical composition comprising, by weight: 0.2 to 0.4% capsaicinextract; 0.8 to 1.6% Cannabis sativa oil; 6 to 12% menthol; 4 to 8% skinpermeator/anti-inflammatory; 2 to 4% analgesic; 2 to 4%analgesic/anti-inflammatory; 1.4 to 2.6% anesthetic; and, 1 to 2%antioxidant.
 10. The composition of claim 9 where the skinpermeator/anti-inflammatory is methyl sulfonyl methane.
 11. Thecomposition of claim 10 where the analgesic is Arnica montana.
 12. Thecomposition of claim 11 where the analgesic/anti-itch/counterirritant iscamphor.
 13. The composition of claim 12 where theanalgesic/anti-inflammatory is Harpagophytim tincture.
 14. Thecomposition of claim 13 where the anesthetic is lidocaine.
 15. Thecomposition of claim 14 where the antioxidant is maqui powder.